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. Author manuscript; available in PMC: 2015 Jan 15.
Published in final edited form as: Bioorg Med Chem Lett. 2013 Dec 11;24(2):548–551. doi: 10.1016/j.bmcl.2013.12.021

Table 1.

Binding affinity and efficacy data for analogues 2–12a

Structure Ki (nM) EC50 (nM) % stimulation
MOR DOR KOR MOR DOR KOR MOR DOR KOR
2 graphic file with name nihms548249t1.jpg 29±9 14±2 310±50 dns dns dns 11±6 dns dns
3 graphic file with name nihms548249t2.jpg 1.4±0.1 7.8±0.9 140±24 dns dns dns dns dns dns
4 graphic file with name nihms548249t3.jpg 2.0±0.8 12±2 110±11 119±39 dns dns 26±2 dns dns
5 graphic file with name nihms548249t4.jpg 3.8±0.8 36±4 250±51 150±49 dns dns 23±2 dns dns
6 graphic file with name nihms548249t5.jpg 1.1±0.3 6.6±2 78±15 85±10 dns dns 17±3 dns dns
7 graphic file with name nihms548249t6.jpg 6.4±0.1 11±0.65 330±92 dns dns dns dns dns dns
8 graphic file with name nihms548249t7.jpg 1.1±0.2 21±7 150±42 dns dns dns dns dns dns
9 graphic file with name nihms548249t8.jpg 0.45±0.3 6.6±2 78±15 64±3 dns dns 43±6 dns 12±1
10 graphic file with name nihms548249t9.jpg 0.29±0.07 23±8.9 89±23 20±3.6 dns 1500±120 36±4 dns 16±3
11 graphic file with name nihms548249t10.jpg 0.3±0.1 28±6.8 54±3.2 41±15 dns dns 49±5 dns 11±7
12 graphic file with name nihms548249t11.jpg 0.42±0.15 6.9±1.7 39±15 53±23 dns 660±80 42±1 dns 12±5
a

All values are expressed as the mean ± SEM of three separate assays performed in duplicate. dns: does not stimulate. Binding affinities (Ki) were obtained by competitive displacement of radiolabeled [3H]diprenorphine in membrane preparations. Efficacy data were obtained using agonist induced stimulation of [35S]GTPγS binding assay. Efficacy is represented as EC50 (nM) and percent maximal stimulation relative to standard agonist DAMGO (MOR), DPDPE (DOR), or U69,593 (KOR) at 10 µM.